AT7867

Description

AT7867 is a potent and orally bioavailable inhibitor of Akt isoforms Akt1, 2, and 3 (IC₅₀s = 32, 17, and 47 nM, respectively). It also inhibits p70S6 kinase and PKA (IC₅₀s = 85 and 20 nM, respectively), but is without effect against a panel of other kinases. AT7867 inhibits growth and induces apoptosis in a variety of cancer cell lines in vitro and suppresses tumor growth of PTEN-deficient xenografts in mice.

The Uses of AT7867

A potent Akt inhibitor with an IC50 of 17 nM. AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50s of 20 nM and 85 nM, respectively.

What are the applications of Application

AT7867 is a potent ATP-competitive inhibitor of Akt1, Akt2 and Akt3

Definition

ChEBI: AT7867 is a member of the class of piperidines carrying two aryl substituents (4-chlorophenyl and 4-(pyrazol-4-yl)phenyl) at position 4. It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor and an antineoplastic agent. It is a member of pyrazoles, a member of piperidines and a member of monochlorobenzenes.

Enzyme inhibitor

This potent ATP-competitive inhibitor (FW = 337.85; CAS 857531-00-1; Solubility: 68 mg/mL DMSO, <1 mg/mL H2O), known systematically as 4- (4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine, targets Akt1, Akt2 and Akt3 Protein Kinases B (or PKB), with IC50 values of 32 nM, 17 nM and 47 nM, respectively. AT7867 also inhibits the structurally related AGC kinases, p70S6K and PKA, with IC50 values of 20 nM and 85 nM, respectively.

References

grimshaw km, hunter lj, yap ta et al. at7867 is a potent and oral inhibitor of akt and p70 s6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. mol cancer ther. 2010 may;9(5):1100-10.